Table 1.
Antiproliferative and CDK2-Cyclin A inhibitory activities of 8-aminoflavopiridol analogues.
| Compounds | ID-8a IC50 (μM) | MCF-7a IC50 (μM) | CDK2-Cyclin A (μM) |
|---|---|---|---|
| Flavopiridol (1) | 0.0070 | 0.026 | 1.5 |
| 17a | 13 | 7.1 | 417 |
| 17b | 5.5 | 4.6 | 417 |
| 17c | 13 | 15 | 217 |
| 17d | 16 | 10 | N.D. |
| 17e | 5.0 | 3.5 | 383 |
| 19a | N.D. | 8.5 | 91 |
| 19b | N.D. | 13 | 339 |
| 19c | N.D. | 9.7 | 90 |
| 19d | N.D. | 13 | 54 |
| 20a | 9.3 | 20 | 417 |
| 20b | 5.7 | 17 | 417 |
| 20c | 7.9 | 20 | 417 |
| 21a | 104 | 5.5 | N.D. |
| 21b | 12 | 4.5 | 417 |
| 21c | 17 | 2.5 | 417 |
| 21d | 13 | 2.8 | N.D. |
| 22a | 9.8 | 5.5 | 417 |
| 22b | 5.3 | 7.1 | 417 |
| 22c | 5.1 | 4.0 | 417 |
| 22d | 6.2 | 20 | N.D. |
| 23 | 18 | 30 | 417 |
| 24a | 16 | 25 | 219 |
| 24b | 9.5 | 16 | 178 |
| 24c | 24 | 17 | 94 |
a
Proliferation experiments were performed as previously described.16
b
CDK2-Cyclin A enzymatic assay is described in the Experimental procedures section. N.D. = not determined.